Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂,竞争性且可逆地抑制 PKCβI 和 PKCβII,IC50 值分别为 4.7 和 5.9 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 453 | 现货 | ||
2 mg | ¥ 659 | 现货 | ||
5 mg | ¥ 1,470 | 现货 | ||
10 mg | ¥ 2,490 | 现货 | ||
25 mg | ¥ 4,260 | 现货 | ||
50 mg | ¥ 6,070 | 现货 | ||
100 mg | ¥ 8,370 | 现货 | ||
500 mg | ¥ 16,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src). |
靶点活性 | PKCη:0.052 μM, PKCβ2:5.9 nM, PKCδ:0.25 μM, PKCγ:0.3 μM, PKCβ1:4.7 nM |
体外活性 | LY333531 strikingly decreases the chance of HUVEC survival and the effect of LY333531 on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, LY333531 reduces the ratio of Bcl-2/Bax. LY333531 can further prompt AGEs-induced endothelial cells apoptosis. The increased expression of Bax, Bad and decreased expression of Bcl-2 and Bcl-2/Bax ratio are associated with the apoptotic process[3]. |
体内活性 | A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin. |
细胞实验 | HUVECs are seeded into 96-well plates in low glucose DMEM with 10% FBS for 12 h. Afterwards, HUVECs are starved for 12 h and incubated with BSA (200 μg/ml), AGEs (200 μg/ml) and LY333531 (200 nM)+AGEs (200 μg/ml) for 48 h. Then, the medium is replaced with 0.5 mg/ml MTT and at 37 ?C in a 95% air/5% CO2 incubator for 4 h. Finally, the medium containing MTT is aspirated and replaced by dimethyl sulphoxide (DMSO). OD is measured with a Microplate spectrophotometer. AGEs:advanced glycation end products.(Only for Reference) |
别名 | Ruboxistaurin, LY333531 HCl, LY 333531 hydrochloride, 芦布妥林 |
分子量 | 505.01 |
分子式 | C28H28N4O3·HCl |
CAS No. | 169939-93-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10.1 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9802 mL | 9.9008 mL | 19.8016 mL | 49.504 mL |
5 mM | 0.396 mL | 1.9802 mL | 3.9603 mL | 9.9008 mL | |
10 mM | 0.198 mL | 0.9901 mL | 1.9802 mL | 4.9504 mL | |
20 mM | 0.099 mL | 0.495 mL | 0.9901 mL | 2.4752 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ruboxistaurin hydrochloride 169939-93-9 Chromatin/Epigenetic Cytoskeletal Signaling PKC Ruboxistaurin Hydrochloride LY 333531 LY333531 Ruboxistaurin LY-333531 LY-333531 Hydrochloride LY 333531 Hydrochloride LY333531 HCl Inhibitor LY 333531 hydrochloride inhibit LY333531 Hydrochloride Protein kinase C 芦布妥林 inhibitor